Over the last several years, a number of high-throughput screening methods have been developed to facilitate the screening of thousands, if not millions, of compounds for a desired activity or activities. Such methods typically are based on detecting the binding of a potentially effective compound to a receptor. While these binding assays are effective at constraining the universe of compounds which may have the desired activity, they typically are not well-suited for evaluating this activity with any degree of detail.
The biological activity of potentially active compounds typically is evaluated using less efficient but more informative “secondary screens” or assays that typically require a substantial input of time by a trained technician or scientist. For evaluation of candidate compounds affecting integral membrane proteins such as receptors and ion channels, the amount of time required per compound may be several hours or days if the assay includes effects on electrophysiological activity. Evaluation of candidate compounds affecting lipid bilayer properties also may be time consuming. Accordingly, there is a need for a more efficient “secondary screen” of compounds affecting the activity of membrane proteins, other lipid bilayer-associated and integral components, including the lipids in the bilayer themselves to identify those few compounds that justify further detailed analysis.